光敏功能化载药系统CPTPP-FA-LCOS的制备及性能

通过酰化反应将叶酸(FA)、两亲性亚油酰化壳寡糖(LCOS)连接到羧基取代的四苯基卟啉(TPP)化合物5-(4-羧基苯基)-10,15,20-三苯基卟啉(CPTPP)结构上,得到了潜在光敏功能化载药系统CPTPP-FA-LCOS。利用FTIR、UV-Vis、TEM、FL对CPTPP-FA-LCOS的结构进行了表征,并运用表面张力法测定了其临界胶束质量浓度(CMC)。结果表明:CPTPP-FA-LCOS的CMC=2.5×10~(-3)g/L,其可形成稳定的球形纳米胶束,粒径在70~120 nm。四唑盐(MTT)比色法的初步实验结果表明:在光照条件下,0.4 g/L的CPTPP-FA-LCOS即可使He La细胞存活率降至50%以下,表明CPTPP-FA-LCOS具有明显的光毒性。

Preparation and Properties of Drug Loading System CPTPP-FA-LCOS with Photosensitive Function

The targeting ligand folic acid (FA) and amphiphilic linoleyl chitosan oligosaccharide (LCOS) with excellent biocompatibility were linked to the carboxyl substituted meso-tetraphenylporphyrin (TPP) of 5-(4-carboxyl)phenyl-10,15,20-triphenyl porphyrin (CPTPP) through acylation reaction. Then the potential drug loading system of CPTPP-FA-LCOS with photosensitive function was obtained. The chemical structure of CPTPP-FA-LCOS was characterized by FTIR, UV-Vis, TEM and fluorescence spectrum. The critical micelle concentration (cmc) of CPTPP-FA-LCOS was also determined using surface tension method. The results showed that cmc value of CPTPP-FA-LCOS was 2.5×10-3 mg/mL. CPTPP-FA-LCOS could be formed into spherical nano-micelles and the particle size was between 70 and 120 nm. The results of preliminary MTT (methyl thiazolyl tetrazolim) suggested that the cell viability was reduced to less than 50% under the light when the concentration of CPTPP-FA-LCOS was 0.4 mg/mL, which suggested the obvious phototoxicity of CPTPP-FA-LCOS.